APETx2 is selective and reversible blocker of acid-sensing ion channel 3 (ASIC3) (ic50 values are 63 and 175 nm for homomeric rat and human asic3 channels). It also inhibits nav1.8 and nav1.2 channels (ic50 values are 55 and 114 nm respectively). It shows analgesic effect on acid induced and inflammatory pain.
CAT No: R0883
CAS No:713544-47-9
Synonyms/Alias:APETx2;713544-47-9;H-Gly-DL-xiThr-DL-Ala-DL-Cys(1)-DL-Ser-DL-Cys(2)-Gly-DL-Asn-DL-Ser-DL-Lys-Gly-DL-xiIle-DL-Tyr-DL-Trp-DL-Phe-DL-Tyr-DL-Arg-DL-Pro-DL-Ser-DL-Cys(3)-DL-Pro-DL-xiThr-DL-Asp-DL-Arg-Gly-DL-Tyr-DL-xiThr-Gly-DL-Ser-DL-Cys(2)-DL-Arg-DL-Tyr-DL-Phe-DL-Leu-Gly-DL-xiThr-DL-Cys(1)-DL-Cys(3)-DL-xiThr-DL-Pro-DL-Ala-DL-Asp-OH;APETx2 TFA;APE-4472-S;NDB54447;AKOS024458355;DA-70987;Gly-Thr-Ala-Cys-Ser-Cys-Gly-Asn-Ser-Lys-Gly-Ile-Tyr-Trp-Phe-Tyr-Arg-Pro-Ser-Cys-Pro-Thr-Asp-Arg-Gly-Tyr-Thr-Gly-Ser-Cys-Arg-Tyr-Phe- Leu-Gly-Thr-Cys-Cys-Thr-Pro-Ala-Asp;
The structural characteristics of APETx2 are compared with that of PcTx1, another effector of ASIC channels but specific to the ASIC1a subtype and to APETx1, a toxin structurally related to APETx2, which targets the HERG potassium channel.
Solution structure of APETx2, a specific peptide inhibitor of ASIC3 proton-gated channels
ASICs appear to be key mediators of inflammatory pain. ASIC antagonists and antisense oligonucleotides reduced both thermal and mechanical hyperalgesia in a rat model of inflammatory pain, highlighting the utility of selective pharmacological agents for studying ASIC channel function. Unfortunately, only two selective ASIC inhibitors have been discovered. The tarantula toxin PcTx1 is a specific blocker of homomeric ASIC1a channels, whereas the sea anemone peptide APETx2 blocks homomeric ASIC3 and ASIC3-containing heteromeric channels. PcTx1 is potently analgesic in mouse models of inflammatory and neuropathic pain, while APETx2 abolishes acid-induced pain in rats. Thus, APETx2 is an invaluable tool for study of ASIC3 channels.
Chemical synthesis and folding of APETx2, a potent and selective inhibitor of acid sensing ion channel 3
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